PE20161405A1 - Analogos de cortistatina y sintesis y usos de los mismos - Google Patents

Analogos de cortistatina y sintesis y usos de los mismos

Info

Publication number
PE20161405A1
PE20161405A1 PE2016000946A PE2016000946A PE20161405A1 PE 20161405 A1 PE20161405 A1 PE 20161405A1 PE 2016000946 A PE2016000946 A PE 2016000946A PE 2016000946 A PE2016000946 A PE 2016000946A PE 20161405 A1 PE20161405 A1 PE 20161405A1
Authority
PE
Peru
Prior art keywords
hydrogen
alkyl
alkenyl
compounds
synthesis
Prior art date
Application number
PE2016000946A
Other languages
English (en)
Inventor
Jae Young Ahn
Juergen Ramharter
Matthew D Shair
Henry Efrem Pelish
Brian Bor-Jen Liau
Original Assignee
Harvard College
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Harvard College filed Critical Harvard College
Publication of PE20161405A1 publication Critical patent/PE20161405A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/22Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/26Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against hormones ; against hormone releasing or inhibiting factors

Abstract

Se refiere a un compuesto de formula A, donde: R1 es hidrogeno, alquilo, alquenilo, entre otros; R2 es hidrogeno, alquilo, alquenilo, entre otros; o R1 y R2 unidos forman un heterociclilo o heteroarilo opcionalmente sustituidos; R3 es hidrogeno o alquilo; R4 es hidrogeno, halogeno, entre otros; R5 es hidrogeno, halogeno o alquilo; los enlaces (a), (b) y (c) representan un enlace sencillo o doble; RB1 y RB2 son independientemente, cuando se presentan, hidrogeno, -XARA, entre otros; XA es –O-, -S-, entre otros; RA es hidrogeno, alquilo, alquenilo, entre otros; o RB1 y RB2 juntos forman un grupo oxo, siempre que al menos uno de RB1 y RB2 no sea hidrogeno. Son compuestos preferidos los compuestos 14B, entre otros. Dichos compuestos son derivados de cortistatina que inhiben la actividad quinasa CDK8 y la proliferacion de las celulas AML, siendo utiles en el tratamiento de afecciones diabeticas, inflamatorias, entre otros
PE2016000946A 2013-12-24 2014-12-24 Analogos de cortistatina y sintesis y usos de los mismos PE20161405A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361920674P 2013-12-24 2013-12-24
US201461935240P 2014-02-03 2014-02-03
US201461993329P 2014-05-15 2014-05-15

Publications (1)

Publication Number Publication Date
PE20161405A1 true PE20161405A1 (es) 2017-01-18

Family

ID=52350382

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016000946A PE20161405A1 (es) 2013-12-24 2014-12-24 Analogos de cortistatina y sintesis y usos de los mismos

Country Status (30)

Country Link
US (3) US9994582B2 (es)
EP (2) EP3087080B1 (es)
JP (2) JP6494631B2 (es)
KR (1) KR20160101162A (es)
CN (2) CN106103452B (es)
AP (1) AP2016009324A0 (es)
AU (2) AU2014369834B2 (es)
BR (1) BR112016014760A2 (es)
CA (1) CA2934819A1 (es)
CL (1) CL2016001631A1 (es)
CR (1) CR20160291A (es)
DO (1) DOP2016000158A (es)
EA (2) EA201891279A1 (es)
EC (1) ECSP16062174A (es)
ES (1) ES2709480T3 (es)
GT (1) GT201600135A (es)
IL (1) IL246390A0 (es)
MD (1) MD20160089A2 (es)
MX (1) MX361652B (es)
MY (1) MY180383A (es)
NI (1) NI201600089A (es)
PE (1) PE20161405A1 (es)
PH (1) PH12016501258A1 (es)
RU (1) RU2016126503A (es)
SA (1) SA516371410B1 (es)
SG (2) SG10201808151RA (es)
SV (1) SV2016005234A (es)
TN (1) TN2016000240A1 (es)
WO (1) WO2015100420A1 (es)
ZA (1) ZA201603894B (es)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201891279A1 (ru) 2013-12-24 2019-01-31 Президент Энд Феллоус Оф Гарвард Колледж Аналоги кортистатина, их синтез и применения
WO2015116904A1 (en) 2014-02-03 2015-08-06 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ror-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
EP3294298A4 (en) 2015-05-08 2018-10-17 President and Fellows of Harvard College Cortistatin analogues, syntheses, and uses thereof
JP2018516884A (ja) * 2015-05-08 2018-06-28 プレジデント アンド フェローズ オブ ハーバード カレッジ コルチスタチン誘導体による治療に対する患者の標的化選択
EP3316889A4 (en) * 2015-07-01 2018-11-14 President and Fellows of Harvard College Cortistatin analogues and syntheses and uses thereof
ES2856931T3 (es) 2015-08-05 2021-09-28 Vitae Pharmaceuticals Llc Moduladores de ROR-gamma
RU2018121946A (ru) 2015-11-20 2019-12-23 Вайтаи Фармасьютиклз, Ллк Модуляторы ror-гамма
SG11201805092WA (en) * 2015-12-23 2018-07-30 Harvard College Cortistatin analogs and uses thereof
WO2017112823A1 (en) * 2015-12-23 2017-06-29 President And Fellows Of Harvard College Targeted selection of patients for treatment with specific cortistatin derivatives
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ROR-γ調節劑
CN109415382A (zh) * 2016-02-19 2019-03-01 哈佛学院院长等 皮质抑素类似物
US11285144B2 (en) 2016-08-03 2022-03-29 The Broad Institute, Inc. Use of CDK8 inhibitors to treat diseases of inflammation and autoimmunity
US11578067B2 (en) 2017-01-30 2023-02-14 Kyoto University Compound, and method for producing regulatory T cells
CN107028956A (zh) * 2017-03-06 2017-08-11 刘杰 一种治疗经期抑郁症的药物组合物
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
MA49685A (fr) 2017-07-24 2021-04-14 Vitae Pharmaceuticals Llc INHIBITEURS DE ROR gamma
JP7285249B2 (ja) 2017-10-02 2023-06-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Cdk8/cdk19阻害剤としての新規な[1,6]ナフチリジン化合物及び誘導体
US11572369B2 (en) 2019-02-01 2023-02-07 University Of South Carolina Bicyclic pyridine compositions and methods of using the same for cancer therapy

Family Cites Families (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2886589A (en) 1957-08-05 1959-05-12 Merck & Co Inc 8-methyl-5-oxyphenyl hexahydroindan compounds
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US4863457A (en) 1986-11-24 1989-09-05 Lee David A Drug delivery device
US4886499A (en) 1986-12-18 1989-12-12 Hoffmann-La Roche Inc. Portable injection appliance
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4853224A (en) 1987-12-22 1989-08-01 Visionex Biodegradable ocular implants
US4997652A (en) 1987-12-22 1991-03-05 Visionex Biodegradable ocular implants
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
US5098443A (en) 1989-03-23 1992-03-24 University Of Miami Method of implanting intraocular and intraorbital implantable devices for the controlled release of pharmacological agents
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5185152A (en) 1990-01-10 1993-02-09 Peyman Gholam A Method and apparatus for controlled release drug delivery to the cornea and anterior chamber of the eye
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5410016A (en) 1990-10-15 1995-04-25 Board Of Regents, The University Of Texas System Photopolymerizable biodegradable hydrogels as tissue contacting materials and controlled-release carriers
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
US5378475A (en) 1991-02-21 1995-01-03 University Of Kentucky Research Foundation Sustained release drug delivery devices
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
IL105050A0 (en) 1992-03-27 1993-07-08 Lilly Co Eli Steroid derivatives
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
US5443505A (en) 1993-11-15 1995-08-22 Oculex Pharmaceuticals, Inc. Biocompatible ocular implants
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
SE9401108D0 (sv) 1994-03-31 1994-03-31 Leiras Oy Ophthalmic composition I
US5725493A (en) 1994-12-12 1998-03-10 Avery; Robert Logan Intravitreal medicine delivery
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
US5847172A (en) 1995-06-07 1998-12-08 Magainin Pharmaceuticals Inc. Certain aminosterol compounds and pharmaceutical compositions including these compounds
US5554187A (en) 1995-08-18 1996-09-10 Rizzo, Iii; Joseph Medication dispensing intra-ocular lens system
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
US6074872A (en) 1996-05-15 2000-06-13 The Scripps Research Institute Cortistatin: nucleic acids that encode these neuropeptides
ZA978537B (en) 1996-09-23 1998-05-12 Focal Inc Polymerizable biodegradable polymers including carbonate or dioxanone linkages.
AU5902398A (en) 1996-12-31 1998-07-31 Human Genome Sciences, Inc. Cortistatin polypeptides
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
US6632457B1 (en) 1998-08-14 2003-10-14 Incept Llc Composite hydrogel drug delivery systems
US20030060425A1 (en) 1998-11-24 2003-03-27 Ahlem Clarence N. Immune modulation method using steroid compounds
US6667299B1 (en) 2000-03-16 2003-12-23 Hollis-Eden Pharmaceuticals, Inc. Pharmaceutical compositions and treatment methods
US6291516B1 (en) 1999-01-13 2001-09-18 Curis, Inc. Regulators of the hedgehog pathway, compositions and uses related thereto
BR0010197A (pt) 1999-04-30 2002-07-16 Arch Dev Corp Derivados de esteróides
DK1955700T3 (da) 1999-09-30 2011-05-23 Harbor Biosciences Inc Terapeutisk behandling af androgenreceptor-betingede lidelser
EP1728797A3 (en) 1999-10-13 2011-03-02 Johns Hopkins University School of Medicine Regulators of the hedgehog pathway, compositions and uses related thereto
EP1223941B1 (en) 1999-10-25 2008-11-05 Hollis-Eden Pharmaceuticals Inc. Therapeutic treatments for blood cell deficiencies using sreroids
CN1827621A (zh) * 2000-03-31 2006-09-06 萨诺化学药物股份公司 雪花胺的新衍生物和类似物
JP2005503425A (ja) 2001-05-24 2005-02-03 アレックザ モレキュラー デリヴァリー コーポレイション 所定の吸入ルートによる薬剤エステルの送出
ITMI20011445A1 (it) 2001-07-06 2003-01-06 Europ Geie Analoghi della cortistantina capaci di legarsi selettivamente ai recettori dei secretagoghi dell'ormone della crescita
WO2003063791A2 (en) 2002-01-30 2003-08-07 Entremed, Inc. Non-steroidal analogs of 2-methoxyestradiol
AU2003292939A1 (en) 2002-12-24 2004-07-22 The University Of British Columbia Angiogenic compounds and uses thereof
BRPI0408703A (pt) 2003-03-24 2006-03-07 Sterix Ltd derivados de estrogênio como inibidores da esteróide sulfatase
JP2006526025A (ja) 2003-05-28 2006-11-16 エントレメッド インコーポレイテッド 抗血管新生剤
WO2005009391A2 (en) * 2003-07-24 2005-02-03 Merck & Co., Inc. Antibiotic compound
US20070004689A1 (en) 2004-03-12 2007-01-04 Agoston Gregory E Antiangiogenic agents
GB0421106D0 (en) 2004-09-22 2004-10-27 Sterix Ltd Compound
CN103349664A (zh) 2005-03-02 2013-10-16 马里兰州立大学巴尔的摩分校 含甾族的c-17苯并吡咯的组合物
MX2008008608A (es) 2006-01-09 2009-03-04 Btg Int Ltd Moduladores de factor i inducible por hipoxia y usos relacionados.
WO2007082980A1 (es) 2006-01-23 2007-07-26 Consejo Superior De Investigaciones Científicas Composiciones y procedimientos para tratar trastornos inflamatorios e inmunitarios con cortistatina
WO2007103162A2 (en) 2006-03-01 2007-09-13 Samaritan Pharmaceuticals, Inc. Structure based drug design of steroidogenesis inhibitors
BRPI0711352A2 (pt) * 2006-05-09 2011-09-27 Merck & Co Inc composto, composição farmacêutica, e, métodos para o antagonismo de atividade receptora de cgrp em um mamìfero, e para, tratar, controlar, melhorar ou reduzir o risco de dor de cabeça, enxaqueca , ou cefaléia vascular
EP1870405A1 (en) * 2006-06-22 2007-12-26 Bioprojet Carbonylated (Aza)cyclohexanes as dopamine D3 receptor ligands
WO2008064425A1 (en) 2006-11-30 2008-06-05 Solbec Pharmaceuticals Limited Glycoalkaloid and chemotherapeutic agent combinations and various uses thereof
CA2674525A1 (en) 2006-12-22 2008-07-03 Albert Einstein College Of Medicine Of Yeshiva University Azetidine analogues of nucleosidase and phosphorylase inhibitors
CA2679845A1 (en) 2007-03-07 2008-09-12 Infinity Discovery, Inc. Cyclopamine lactam analogs and methods of use thereof
WO2009046314A2 (en) * 2007-10-04 2009-04-09 President And Fellows Of Harvard College Moenomycin analogs, methods of synthesis, and uses thereof
CA2723689C (en) * 2008-05-05 2016-07-05 Ryan A. Shenvi Synthesis of (+) cortistatin a and related compounds
WO2010024930A2 (en) * 2008-08-28 2010-03-04 President And Fellows Of Harvard College Cortistatin analogues and syntheses therof
JP2012524778A (ja) 2009-04-22 2012-10-18 プレジデント アンド フェロウズ オブ ハーバード カレッジ 血管新生阻害剤
US8598344B2 (en) 2009-11-30 2013-12-03 Senex Biotechnology CDKI pathway inhibitors and uses thereof
BR112012029437A2 (pt) 2010-05-20 2017-03-07 F Hoffmann - La Roche Ag derivados de pirrolo[2,3-b]pirazina-7-carboxamida e seu uso como inibidores de jak e syk
EP2617720B1 (en) 2010-09-17 2016-03-30 Osaka University Novel cortistatin a analog and use thereof
WO2012096934A2 (en) 2011-01-10 2012-07-19 The Scripps Research Institute Inhibitors of retroviral replication
KR20150023223A (ko) 2012-02-02 2015-03-05 세넥스 바이오테크놀러지 인코포레이티드 Cdk8/cdk19 선택성 억제제 및 암에 대한 항-전이 및 화학예방 방법에서 이들의 용도
WO2013122609A1 (en) 2012-02-17 2013-08-22 Genentech, Inc. Methods of using cdk8 antagonists
WO2014123900A1 (en) 2013-02-05 2014-08-14 Sirenas Marine Discovery Anti-cancer and anti-hiv compounds
WO2014134169A1 (en) 2013-02-26 2014-09-04 Senex Biotechnology, Inc. Inhibitors of cdk8/19 for use in treating estrogen receptor positive breast cancer
WO2014199377A1 (en) 2013-06-10 2014-12-18 Yeda Research And Development Co. Ltd. Compositions and methods for treating a hematological malignancy associated with an altered runx1 activity or expression
PT3046933T (pt) 2013-09-18 2019-05-31 Bcn Peptides Sa Análogos de cortistatina para o tratamento de doenças inflamatórias e/ou imunitárias
EA201891279A1 (ru) 2013-12-24 2019-01-31 Президент Энд Феллоус Оф Гарвард Колледж Аналоги кортистатина, их синтез и применения

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CN110183461A (zh) 2019-08-30
AU2014369834B2 (en) 2018-12-20
US10273241B2 (en) 2019-04-30
SG11201605178WA (en) 2016-07-28
CR20160291A (es) 2017-02-24
AP2016009324A0 (en) 2016-07-31
NI201600089A (es) 2016-08-18
JP2019108367A (ja) 2019-07-04
EA030907B1 (ru) 2018-10-31
BR112016014760A2 (pt) 2017-12-12
RU2016126503A3 (es) 2018-07-17
EP3505521A1 (en) 2019-07-03
MY180383A (en) 2020-11-28
MD20160089A2 (ro) 2016-12-31
JP6494631B2 (ja) 2019-04-03
CN106103452A (zh) 2016-11-09
EP3087080B1 (en) 2018-11-28
KR20160101162A (ko) 2016-08-24
DOP2016000158A (es) 2016-10-16
CA2934819A1 (en) 2015-07-02
MX361652B (es) 2018-12-13
EP3087080A1 (en) 2016-11-02
RU2016126503A (ru) 2018-01-30
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IL246390A0 (en) 2016-08-31
ES2709480T3 (es) 2019-04-16
JP2017509586A (ja) 2017-04-06
US20180319814A1 (en) 2018-11-08
AU2019201888A1 (en) 2019-04-11
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US9994582B2 (en) 2018-06-12
ECSP16062174A (es) 2018-12-31
EA201891279A1 (ru) 2019-01-31
CL2016001631A1 (es) 2017-02-24
WO2015100420A1 (en) 2015-07-02
TN2016000240A1 (en) 2017-10-06
EA201691167A1 (ru) 2016-11-30
US10508121B2 (en) 2019-12-17
US20170029435A1 (en) 2017-02-02
AU2014369834A1 (en) 2016-06-23
MX2016008436A (es) 2016-12-16
SG10201808151RA (en) 2018-10-30
ZA201603894B (en) 2018-08-29
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GT201600135A (es) 2018-11-27
CN106103452B (zh) 2019-05-21

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